Functional organisation and gain of activity: The case of the antibacterial tetra-para-guanidinoethyl-calix[4]arene
| Autor: | Raphaël E. Duval, Maxime Mourer, Jean-Bernard Regnouf-de-Vains, Chantal Finance |
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| Přispěvatelé: | Structure et Réactivité des Systèmes Moléculaires Complexes (SRSMC), Université de Lorraine (UL)-Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC) |
| Rok vydání: | 2006 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Molecular Conformation Pharmaceutical Science Microbial Sensitivity Tests 010402 general chemistry Guanidines 01 natural sciences Biochemistry Chemical synthesis Inclusion compound Diffusion chemistry.chemical_compound [SDV.SP.MED]Life Sciences [q-bio]/Pharmaceutical sciences/Medication Tetramer Drug Discovery Calixarene Molecular Biology ComputingMilieux_MISCELLANEOUS Antibacterial agent biology 010405 organic chemistry Organic Chemistry biology.organism_classification [SDV.MP.BAC]Life Sciences [q-bio]/Microbiology and Parasitology/Bacteriology Anti-Bacterial Agents 0104 chemical sciences Monomer chemistry [SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/Virology Molecular Medicine Tetra Cyclophane |
| Zdroj: | Bioorganic and Medicinal Chemistry Letters Bioorganic and Medicinal Chemistry Letters, Elsevier, 2006, 16 (11), pp.2960-2963. ⟨10.1016/j.bmcl.2006.02.072⟩ |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2006.02.072 |
| Popis: | The antibacterial activities of the para-guanidinoethylphenol and of its cyclic tetramer, the tetra-para-guanidinoethyl-calix[4]arene, have been evaluated on reference gram-positive and gram-negative bacteria. Antibiotic disk diffusion assays completed by micromethod technique were employed to determine if a synergistic effect could be expected from the spatial organisation of the monomer into its cyclic tetrameric analogue. Disk diffusion assays and microdilution experiments revealed better properties for the calixarene species, with a real and important gain of activity with regards to the monomer. |
| Databáze: | OpenAIRE |
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